不同赋形剂在聚氧乙烯和黄原胶基质中的药物释放动力学比较分析

Haja Muhamad, Nihad Mawla, Saedah Dereiah, Adam Ward, James Williamson and Kofi Asare-Addo
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引用次数: 0

摘要

本研究以盐酸心得安(PPN)为模型药物,考察了不同药用辅料对聚氧乙烯(PEO) -黄原胶(XG)缓释制剂的药物释放动力学的影响。配方中PEO或XG与乳糖、二碱性磷酸钙(DCP)或微晶纤维素(MCC)的比例分别为1:3、1:1和3:1 w/w。压实分析表明,含有较高赋形剂含量的配方孔隙率增加,硬度值降低。接触角测量表明,辅料含量高的配方,特别是含有乳糖的配方,接触角较低,这表明亲水性增加。体外溶出实验完成后,分析溶出效率(DE)、平均溶出时间(MDT)、平均溶出速率(MDR)和相似因子(f2)。结果表明,在PEO和XG配方中添加更多的乳糖均能加快药物释放速度,PEO:乳糖1:3的DE最高(64±8%),MDT最短(77±10 min)。同样,与PEO配方相比,XG:乳糖1:3比例的DE最高(61±2%),MDR最快(0.20±0.01% min−1),但效果不明显。动力学分析表明,大多数pepeo配方遵循Peppas模型,表明扩散和聚合物侵蚀机制驱动的非菲克输运。然而,大多数XG公式遵循Higuchi模型。相似因子(f2)揭示了辅料种类和配比对溶出度的影响。含有较多MCC的配方与纯聚合物的相似度较高。这些结果为赋形剂如何用于优化聚合物基质以调节缓释制剂中的药物释放提供了重要的见解。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Comparative analysis of drug release kinetics in polyethylene oxide and xanthan gum matrices with various excipients

Comparative analysis of drug release kinetics in polyethylene oxide and xanthan gum matrices with various excipients

This study aimed to investigate the effect of various pharmaceutical excipients on the drug release kinetics of extended-release formulations composed of polyethylene oxide (PEO) and xanthan gum (XG), using propranolol hydrochloride (PPN) as the model drug. The formulations contained different ratios (1 : 3, 1 : 1, and 3 : 1 w/w) of PEO or XG to either lactose, dibasic calcium phosphate (DCP), or microcrystalline cellulose (MCC). Compaction analysis revealed that formulations that contain higher excipient content exhibit increased porosity and decreased hardness values. Contact angle measurements indicated that formulations with higher excipient content, particularly with lactose, displayed lower contact angles, which is indicative of increased hydrophilicity. After the in vitro dissolution studies were conducted, the dissolution efficiency (DE), mean dissolution time (MDT), mean dissolution rate (MDR), and similarity factors (f2) were analysed. The findings showed that a higher amount of lactose in both PEO and XG formulations resulted in faster drug release, with the PEO : lactose 1 : 3 ratio achieving the highest DE (64 ± 8%) and the shortest MDT (77 ± 10 min). Similarly, the XG : lactose 1 : 3 ratio exhibited the highest DE (61 ± 2%) and fastest MDR (0.20 ± 0.01% min−1), although the effect was less pronounced compared to PEO formulations. The kinetic analysis showed that most PEO formulations followed the Peppas model, indicating non-Fickian transport driven by both diffusion and polymer erosion mechanisms. However, most of the XG formulations followed the Higuchi model. The similarity factors (f2) revealed the influence of excipient type and ratio on the dissolution profiles. Formulations containing a higher amount of MCC displayed higher similarity with the pure polymer profiles. These results give important insights into how excipients can be used to optimise polymeric matrices to regulate drug release in extended-release formulations.

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